Boron Trichloride → HCID 58655382, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of compound 1-6 from Step F (1 eq) in dichloromethane at −78° C. is added boron trichloride (1M in dichloromethane, 10 eq) dropwise. The mixture is stirred at −78° C. then at −30° C. to −20° C. The reaction is quenched by addition of methanol/dichloromethane (1:1) and the resulting mixture stirred at −15° C., then neutralized with aqueous ammonia at 0° C. and stirred at room temperature. The solid is filtered and washed with CH2Cl2/MeOH (1/1). The combined filtrate and washings are evaporated, and the residue is purified by flash chromatography over silica gel using CH2Cl2 and CH2Cl2:MeOH gradient as the eluent to furnish the title compound 1-7.

Provenance & Evidence